Santaris Pharma A/s

Roche Innovation Center Copenhagen A/s

Beijing University of Technology

Adelaide Research & Innovation Pty Ltd

Daniel Sejer Pedersen

Troels Koch

Christoph Rosenbohm

Signe M Christensen

Henrik Frydenlund Hansen

Charlotte Albaek Thrue

Majken Westergaard

Miriam Frieden

Nikolaj Dam Mikkelsen

Jesper Wengel

Mads Detlef Sørensen

Matthew Wilce

Nicole Pendini

Andrew Abell

Steven Polyak

Min Yin Yap

Grant Booker

Mads Detlef Sorensen

John Wallace

Christoph Rosenbohn

Tatiana Soares Da Costa

Angie Jarrad

William Tieu

Kelly Lee Keeling

Charlotte Thrue

A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.

Antisense design

A new class of biotin protein ligase (BPL) inhibitors that have antibacterial activity against multipleisolates, including clinically important methicillin-resistant(MRSA) are disclosed that are non-toxic.

Antimicrobial compounds

Amino-LNA, thio-LNA and alpha-L-oxy-LN

The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as &#x3b1;--oxy-LNA, amino-LNA, &#x3b1;--amino-LNA, thio-LNA, &#x3b1;--thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues. 

Synthesis of locked nucleic acid derivatives

Methods are described for the synthesis of Locked Nucleic Acid (LNA) derivatives using certain nitrogen-containing nucleophiles.

The present invention is directed to novel oligonucleotides with improved antisense properties. The novel oligonucleotides comprise at least one Locked Nucleic Acid (LNA) selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides. The present invention also provides a new class of pharmaceuticals which comprise antisense oligonucleotides and are useful in antisense therapy.

Oligonucleotides with alternating segments of locked and non-locked nucleotides

The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as &#x3b1;--oxy-LNA, amino-LNA, &#x3b1;--amino-LNA, thio-LNA, &#x3b1;--thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilizing intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues. 

The present invention relates to large scale preparation of LNA phosphoramidites using a 2-cyanoethyl-N,N,N',N&#x2032;-tetra-substituted phosphoramidite and a nucleophilic activator, e.g. 2-cyanoethyl-N,N,N&#x2032;,N&#x2032;-tetraisopropylphosphoramidite and 4,5-dicyanoimidazole. The method is faster and more cost efficient that previously known methods.

Method for preparation of LNA phosphoramidites

Growing community of inventors

Valby, Denmark

Daniel Sejer Pedersen